Design and Discovery of New Dual Carbonic Anhydrase IX and VEGFR‐2 Inhibitors Based on the Benzenesulfonamide‐Bearing 4‐Thiazolidinones/2,4‐Thiazolidinediones Scaffold DOI Open Access
Merve Zengin, Oya Ünsal Tan, Suna Sabuncuoğlu

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 85(8)

Published: Dec. 1, 2024

Dual-targeting drug design has become a popular approach in investigating and developing potent anticancer agents. In this regard, carbonic anhydrase (CAIX) vascular endothelial growth factor receptor (VEGFR-2) are emerging as highly effective targets the battle against cancer. present study, two series of 4-thiazolidinones/2,4-thiazolidinediones carrying 2-methylbenzenesulfonamide derivatives were designed synthesized potential dual CAIX/VEGFR-2 inhibitors. All target compounds evaluated CAIX enzyme compared to dorzolamide acetazolamide, subsequently most inhibitors (3a, 3b, 3o, 6d, 6g, 6i) selected evaluate their inhibitory activity VEGFR-2 using sorafenib reference drug. These also MCF-7 breast cancer cells murine fibroblast 3T3 cell line. According results, 3b (CAIX IC

Language: Английский

Supramolecular complex catalyzed green synthesis of 9-(2-Ethylhexyl) carbazole: Structural, optical and DFT investigations DOI
Priyanka Behera,

T. Jaison Jose,

D.S. Ramakrishna

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1308, P. 138089 - 138089

Published: March 19, 2024

Language: Английский

Citations

22
Recent Advances in Structural Optimization of Quinazoline-Based Protein Kinase Inhibitors for Cancer Therapy (2021–Present) DOI Creative Commons
Heba T. Abdel‐Mohsen, Manal M. Anwar, Nesreen S. Ahmed

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(4), P. 875 - 875

Published: Feb. 16, 2024

Cancer is a complicated, multifaceted disease that can impact any organ in the body. Various chemotherapeutic agents have low selectivity and are very toxic when used alone or combination with others. Resistance one of most important hurdles develop due to use many anticancer therapeutics. As result, treating cancer requires target-specific palliative care strategy. Remarkable scientific discoveries shed light on several molecular mechanisms underlying cancer, resulting development various targeted agents. One heterocyclic motifs quinazoline, which has wide range biological uses chemical reactivities. Newer, more sophisticated medications quinazoline structures been found last few years, great strides made creating effective protocols for building these pharmacologically active scaffolds. A new class known as quinazoline-based derivatives possessing properties consists well-known compounds block different protein kinases other targets. This review highlights recent updates (2021–2024) acting against chemotherapeutics. It also provides guidance design synthesis novel analogues could serve lead compounds.

Language: Английский

Citations

10
Anticancer evaluations of iodoquinazoline substituted with allyl and/or benzyl as dual inhibitors of EGFRWT and EGFRT790M: design, synthesis, ADMET and molecular docking DOI Creative Commons
Ahmed K. B. Aljohani, Khaled El‐Adl, Basmah Almohaywi

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(12), P. 7964 - 7980

Published: Jan. 1, 2024

Fifteen new iodoquinazoline derivatives, 5a,b to 18, are reported in this study and their anticancer evaluation as dual inhibitors of EGFR WT T790M .

Language: Английский

Citations

5
Utility of sulfachloropyridazine in the synthesis of novel anticancer agents as antiangiogenic and apoptotic inducers DOI

Sally S. Zahran,

Fatma A. Ragab,

Aiten M. Soliman

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 148, P. 107411 - 107411

Published: April 30, 2024

Language: Английский

Citations

5
Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET, molecular docking and dynamic simulation DOI Creative Commons

Hatem Hussein Bayoumi,

Mohamed‐Kamal Ibrahim,

Mohammed A. Dahab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(30), P. 21668 - 21681

Published: Jan. 1, 2024

Novel phthalazine derivatives were designed, synthesized and evaluated against Hep G2 MCF-7 as VEGFR-2 inhibitors.

Language: Английский

Citations

4
Design and Synthesis of Novel Thiazolo[5,4-b]pyridine Derivatives as Potent and Selective EGFR-TK Inhibitors Targeting Resistance Mutations in Non-Small Cell Lung Cancer DOI

Avinash S. Borude,

Santosh Rangnath Deshmukh,

Shailee V. Tiwari

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 276, P. 116727 - 116727

Published: July 30, 2024

Language: Английский

Citations

4
Rational design, docking, syntheses, ADMET and cytotoxicity assessments of iodoquinazoline derivatives as inhibitors of EGFRT790M and VEGFR-2 DOI
Ahmed K. B. Aljohani, Marwa Alsulaimany,

Omar M. Alatawi

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141634 - 141634

Published: Jan. 1, 2025

Language: Английский

Citations

0
Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition DOI Creative Commons
Mohamed S. Nafie, Sherif Ashraf Fahmy,

Shaima H. Kahwash

et al.

RSC Advances, Journal Year: 2025, Volume and Issue: 15(7), P. 5597 - 5638

Published: Jan. 1, 2025

This is an updated review for the anticancer activity of benzodiazine heterocyclic derivatives through kinase inhibition.

Language: Английский

Citations

0
Sulfonamides a Promising Hit for Cancer Therapy Through VEGFR-2 Inhibition DOI Creative Commons

Eleftherios Charissopoulos,

Eleni Pontiki

Biomedicines, Journal Year: 2025, Volume and Issue: 13(4), P. 772 - 772

Published: March 21, 2025

Vascular endothelial growth factor receptor-2 (VEGFR-2), a tyrosine kinase receptor (TKR), plays crucial role in angiogenesis and is overexpressed most cancers. It important for tumor angiogenesis, facilitating essential angiogenic cellular processes, such as promoting cell survival, proliferation, migration, vascular permeability. Consequently, VEGFR-2 has become one of the main targets anti-angiogenic therapy, with its inhibition serving strategy developing new drugs to mitigate angiogenesis-dependent Small-molecule targeting VEGFR-2, approved by USFDA, are exhibiting development drug resistance during chemotherapy, cardiac-related side effects being consistently reported. In conclusion, it develop novel strategies enhance efficacy inhibitors eliminate their adverse effects. Multifunctional that target multiple pathways present promising strategy, enhancing while minimizing Sulfonamide derivatives extensively used medicinal chemistry modern discovery due variety pharmacological activities. The review focuses on compounds endowed potential inhibition, four which additionally carbonic anhydrase inhibitory activity.

Language: Английский

Citations

0
Iodoquinazoline-derived VEGFR-2 and EGFRT790M dual inhibitors: Design, synthesis, molecular docking and anticancer evaluations DOI
Abeer A. Mohamed,

Sanadelaslam S. A. El‐Hddad,

Ahmed K. B. Aljohani

et al.

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 143, P. 107062 - 107062

Published: Dec. 25, 2023

Language: Английский

Citations

9